Patent classifications
C07D209/14
SELECTIVE HDAC6 INHIBITORS AND USES THEREOF
The present invention relates to selective Histone deacetylase 6 (HDAC6) inhibitors and compositions containing the same. Methods of treating diseases and conditions wherein inhibition of HDAC6 provides a benefit, like a cell proliferative disease, an autoimmune or inflammatory disorder, a neurodegenerative disease, or a combination thereof, also are disclosed.
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SELECTIVE HDAC6 INHIBITORS AND USES THEREOF
The present invention relates to selective Histone deacetylase 6 (HDAC6) inhibitors and compositions containing the same. Methods of treating diseases and conditions wherein inhibition of HDAC6 provides a benefit, like a cell proliferative disease, an autoimmune or inflammatory disorder, a neurodegenerative disease, or a combination thereof, also are disclosed.
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Fluorescent metal ion indicators with large stokes shifts
The present invention provides fluorogenic compounds for the detection of target metal ions wherein the compounds exhibit a Stokes shift greater than 50 nm and the detectable signal is modulated by photoinduced electron transfer (PET). The present compounds consist of three functional elements, the ion sensing moiety (chelating moiety), the reporter moiety (fluorophore or fluorescent protein) and spacer or linker between the sensing and reporter moieties of the present compound that allows for PET upon binding of a metal ion and excitation by an appropriate wavelength.
Fluorescent metal ion indicators with large stokes shifts
The present invention provides fluorogenic compounds for the detection of target metal ions wherein the compounds exhibit a Stokes shift greater than 50 nm and the detectable signal is modulated by photoinduced electron transfer (PET). The present compounds consist of three functional elements, the ion sensing moiety (chelating moiety), the reporter moiety (fluorophore or fluorescent protein) and spacer or linker between the sensing and reporter moieties of the present compound that allows for PET upon binding of a metal ion and excitation by an appropriate wavelength.
Hydrazinyl-indole compounds and methods for producing a conjugate
The present disclosure provides conjugate structures (e.g., polypeptide conjugates) and hydrazinyl-indole compounds used to produce these conjugates. The disclosure also provides methods of production of such conjugates, as well as methods of using the same.
ArylSulfonamide-based matrix metalloprotease inhibitors
The present invention provides a compound of formula (I): ##STR00001##
said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
SYNTHESIS METHOD OF INDOLE DERIVATIVE CAPABLE OF EFFICIENTLY DEGRADING PERFLUORINATED COMPOUND (PFC) AND THE USE OF THE INDOLE DERIVATIVE
A synthesis method of an indole derivative capable of efficiently degrading a perfluorinated compound (PFC) and a use of the indole derivative are provided. The synthesis method includes dissolving an appropriate amount of indole, alkylamine, and formaldehyde in an ethanol solution, conducting a reaction at reflux under suitable conditions for a specified period of time with ZnCl.sub.2 or glacial acetic acid as a catalyst to form a reaction product, vacuum-drying the reaction product, and purifying the reaction product through column chromatography to obtain a novel indole derivative with a hydrophobic alkyl branch. The present indole derivative has some hydrophobicity and a positively charged amino group that can effectively capture PFCs in contaminated water to produce a sub-nanoscale self-assembled aggregate. Hydrated electrons generated by light irradiation can directly attack PFCs in the aggregate without long-distance mass transfer, improving the utilization rate of hydrated electrons and reduces the ratio of fed materials.
SYNTHESIS METHOD OF INDOLE DERIVATIVE CAPABLE OF EFFICIENTLY DEGRADING PERFLUORINATED COMPOUND (PFC) AND THE USE OF THE INDOLE DERIVATIVE
A synthesis method of an indole derivative capable of efficiently degrading a perfluorinated compound (PFC) and a use of the indole derivative are provided. The synthesis method includes dissolving an appropriate amount of indole, alkylamine, and formaldehyde in an ethanol solution, conducting a reaction at reflux under suitable conditions for a specified period of time with ZnCl.sub.2 or glacial acetic acid as a catalyst to form a reaction product, vacuum-drying the reaction product, and purifying the reaction product through column chromatography to obtain a novel indole derivative with a hydrophobic alkyl branch. The present indole derivative has some hydrophobicity and a positively charged amino group that can effectively capture PFCs in contaminated water to produce a sub-nanoscale self-assembled aggregate. Hydrated electrons generated by light irradiation can directly attack PFCs in the aggregate without long-distance mass transfer, improving the utilization rate of hydrated electrons and reduces the ratio of fed materials.
Fused bicyclic alkylene linked imidodicarbonimidic diamides, methods for synthesis, and uses in therapy
The present invention provides novel fused bicyclic alkylene linked imidodicarbonimidic diamides. In particular, described herein are N-[2-(indol-3-yl)alkylene]-linked imidodicarbonimidic diamides and N-[2-(pyrrolopyridin-3-yl)alkylene]-linked imidodicarbonimidic diamides (compound of formula (I) or formula (II)), and uses therefor. The compounds of the present invention are believed to be organic cation transporter selective compounds, useful for the treatment of diseases and conditions caused by reduced activity of 5′ adenosine monophosphate-activated protein kinase (AMPK).
Method of synthesizing near IR, closed chain sulfo-cyanine dyes
Compositions and methods of synthesizing near IR, closed chain, sulfo-cyanine dyes are provided.